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Purity: ≥98%
Peficitinib (formerly ASP015K and JNJ54781532) is a novel, potent and orally bioavailable inhibitor of Janus kinase-JAK with potential anti-inflammatory activities. It inhibits JAK1, JAK2, JAK3 and Tyk2 with IC50 values of 3.9, 5.0, 0.7 and 4.8 nM, respectively. It exhibited potent in vivo anti-rheumatoid arthritis (RA) efficacy in adjuvant-induced arthritis model in rats. In addition, ASP-015K inhibited the IL-2-induced proliferation of human T cells with IC50 of 18 nM.
| ln Vitro |
In a concentration-dependent manner, peficitinib hydrobromide (0-100 nM; 3 days) suppresses T cell proliferation driven by IL-2[1]. With a mean IC50 of 124 nM in rat whole blood and a mean IC50 of 127 nM in human cells, peficitinib hydrobromide (10-1000 nM) suppresses IL-2-induced STAT5 phosphorylation in a concentration-dependent manner[1].
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| ln Vivo |
In an adjuvant-induced arthritic rat model, peficitinib hydrobromide (1-30 mg/kg; po; once daily for 24 days) exhibits dose-dependent effectiveness in both preventative and therapeutic dosage regimens[1].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: Splenocytes from male Lewis rats Tested Concentrations: 0 -100 nM Incubation Duration: 3 days Experimental Results: Inhibited IL-2-induced T cell proliferation in a concentration-dependent manner with an IC50 of 10 nM. |
| Animal Protocol |
Animal/Disease Models: Seven-weeks-old female Lewis rats, adjuvant-induced arthritis (AIA) model[1]
Doses: 1, 3, 10, and 30 mg/kg Route of Administration: Oral administration, one time/day for 24 days Experimental Results: Dramatically inhibited the increase in paw volume at doses of 1 mg/kg or greater with an ED50 value of 2.7 mg/kg (95% confidence interval: 1.5–4.2 mg/kg). Dramatically decreased the bone destruction score at 10 mg/kg or greater and almost fully ameliorated both paw swelling and bone destruction scores at 30 mg/kg. |
| References |
[1]. Ito M, et al. A novel JAK inhibitor, peficitinib, demonstrates potent efficacy in a rat adjuvant-induced arthritis model. J Pharmacol Sci. 2017 Jan;133(1):25-33.
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| Molecular Formula |
C18H22N4O2
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| Molecular Weight |
326.39
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| CAS # |
944118-01-8
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| Related CAS # |
Peficitinib hydrobromide;1353219-05-2;Peficitinib hydrochloride;1353219-06-3
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| SMILES |
O([H])C12C([H])([H])C3([H])C([H])([H])[C@]([H])(C1([H])[H])C([H])([C@@]([H])(C3([H])[H])C2([H])[H])N([H])C1C(C(N([H])[H])=O)=C([H])N=C2C=1C([H])=C([H])N2[H]
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0638 mL | 15.3191 mL | 30.6382 mL | |
| 5 mM | 0.6128 mL | 3.0638 mL | 6.1276 mL | |
| 10 mM | 0.3064 mL | 1.5319 mL | 3.0638 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03971253 | Recruiting | Drug: Peficitinib | Rheumatoid Arthritis (RA) | Astellas Pharma Inc | September 2, 2019 | |
| NCT04143477 | Completed | Drug: peficitinib | Healthy Volunteers | Astellas Pharma China, Inc. | December 5, 2019 | Phase 1 |
| NCT02531191 | Completed | Drug: peficitinib | Healthy Volunteers | Astellas Pharma Inc | June 21, 2015 | Phase 1 |
| NCT02111317 | Completed | Drug: ASP015K Drug: verapamil |
Healthy Subjects Pharmacokinetics of ASP015K |
Astellas Pharma Global Development, Inc. |
October 2013 | Phase 1 |
American College of Rheumatology (ACR) response rates at week 12 (full analysis set population).Ann Rheum Dis.2016 Jun;75(6):1057-64. |
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COA
Efficacy variables of mean changes from baseline in the (A) ACR20, (B) DAS28-CRP, (C) HAQ-DI and (D) CRP over time.